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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
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G Protein-coupled Receptors01:15

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Transducer Mechanism: G Protein–Coupled Receptors01:30

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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...
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G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
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G-protein Coupled Receptors01:21

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Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

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Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high...
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Computational methods for studying G protein-coupled receptors (GPCRs).

Agnieszka A Kaczor1, Ewelina Rutkowska2, Damian Bartuzi3

  • 1Department of Synthesis and Chemical Technology of Pharmaceutical Substances with Computer Modelling Lab, Faculty of Pharmacy with Division of Medical Analytics, Medical University of Lublin, Lublin, Poland; School of Pharmacy, University of Eastern Finland, Kuopio, Finland.

Methods in Cell Biology
|March 2, 2016
PubMed
Summary

New insights into G protein-coupled receptors (GPCRs) reveal complex signaling mechanisms. Computational methods enhance drug design for GPCR-targeting therapies, improving safety and efficacy.

Keywords:
Biased signalingGPCR dimersGPCRsHomology modelingMolecular dockingMolecular dynamicsQuantitative structure–activity relationshipVirtual screening

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Area of Science:

  • Pharmacology
  • Computational Biology
  • Medicinal Chemistry

Background:

  • G protein-coupled receptors (GPCRs) traditionally function via the ternary complex model involving receptor, agonist, and G protein.
  • GPCR activation by agonists initiates intracellular signaling cascades through G proteins.
  • Recent discoveries reveal novel GPCR signaling mechanisms beyond the classical model.

Purpose of the Study:

  • To explore advanced findings in GPCR functioning and their implications for drug design.
  • To highlight the role of computational methods in studying complex GPCR behaviors.
  • To underscore the potential for developing safer and more effective GPCR-targeting drugs.

Main Methods:

  • Review of extensive studies on GPCR signaling.
  • Application of computational methods including virtual screening, homology modeling, molecular dynamics, and QSAR.
  • Analysis of novel signaling mechanisms like ligand promiscuity, allosteric modulation, biased agonism, and receptor oligomerization.

Main Results:

  • Discovery of complex GPCR signaling pathways, including ligand promiscuity, signaling cross-talks, and biased agonism.
  • Identification of receptor homo- and heterodimerization and oligomerization as significant functional units.
  • Demonstration of computational techniques' efficiency in studying GPCRs and identifying drug leads.
  • Virtual screening techniques show particular efficacy for GPCRs compared to water-soluble proteins.

Conclusions:

  • Advanced understanding of GPCRs opens new avenues for drug design.
  • Computational approaches significantly aid in discovering compounds with tailored affinity profiles.
  • GPCR-targeting drugs can be developed with improved safety and efficacy profiles through modern drug design strategies.